Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents

Zhang, Juan; Liu, Xuliang; Sa, Na; Zhang, Jin-He; Cai, Yong-Si; Wang, Kai-Ming; Xu, Wei; Jiang, Cheng-Shi; Zhu, Kong-Kai

doi:10.1016/j.ejmech.2024.116341

Cited by 3 publications

(1 citation statement)

References 48 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The most potential compound showed good PRMT5/ EGFR inhibitory activities, with IC 50 values of 15.47 � 1.31 and 19.31 � 2.14 μM, respectively. [81] On the other hand, tetrahydro-β-carbolines with simple substituted groups at carbon atoms of the ring fragment were found to widely exist in some fruits and fruit juices (Figure 6). For example, 1-methyl-tetrahydro-β-carboline, 6-hydroxy-1-methyl-tetrahydro-β-carboline, and 1-methyl-tetrahydro-β-carboline-3-carboxylic acid were found in the fruits including tomato, bananas, pineapple, oranges, grapefruits and so on.…”

Section: C-substituted Tetrahydro-β-carbolinesmentioning

confidence: 99%

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Du,

Semghouli,

Mei

et al. 2024

Adv Synth Catal

View full text Add to dashboard Cite

Abstract. Tetrahydro‐β‐carbolines (THβCs) also known as tryptolines serve as important structural elements in natural products and pharmaceutical compounds, and they are also utilized in drug discovery. They display diverse bioactivities, including anticancer, antifungal, antiparasitic, anti‐ischemic, anti‐inflammatory, and other activities. Besides their pharmacological and biological significance, these structural motifs are also extensively used in the production of other bioactive compounds. This review is intended to summarize recent advancements in the chemistry of this compound class, including the synthesis and the applications as organic synthetic intermediates and bioactive molecules.

show abstract

Section: C-substituted Tetrahydro-β-carbolinesmentioning

confidence: 99%

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Du,

Semghouli,

Mei

et al. 2024

Adv Synth Catal

View full text Add to dashboard Cite

show abstract

Tetrahydrocarbazoles incorporating 5-arylidene-4-thiazolinones as potential antileukemia and antilymphoma targeting tyrosine kinase and tubulin polymerase enzymes: Design, synthesis, structural, biological and molecular docking studies

Ali,

Mohammed,

Kariuki

et al. 2024

Bioorganic Chemistry

View full text Add to dashboard Cite

Synthesis and Biological Activities of C1-Substituted Acylhydrazone β-Carboline Analogues as Antifungal Candidates

Xu,

Li,

Zhang

et al. 2024

Molecules

View full text Add to dashboard Cite

In our ongoing work to create potential antifungal agents, we synthesized and tested a group of C1-substituted acylhydrazone β-carboline analogues 9a–o and 10a–o for their effectiveness against Valsa mali, Fusarium solani, Fusarium oxysporum, and Fusarium graminearum. Their compositions were analyzed using different spectral techniques, such as 1H/13C NMR and HRMS, with the structure of 9l being additionally confirmed through X-ray diffraction. The antifungal evaluation showed that, among all the target β-carboline analogues, compounds 9n and 9o exhibited more promising and broad-spectrum antifungal activity than the commercial pesticide hymexazol. Several intriguing findings regarding structure–activity relationships (SARs) were examined. In addition, the cytotoxicity test showed that these acylhydrazone β-carboline analogues with C1 substitutions exhibit a preference for fungi, with minimal harm to healthy cells (LO2). The reported findings provide insights into the development of β-carboline analogues as new potential antifungal agents.

show abstract

Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents

Cited by 3 publications

References 48 publications

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

Tetrahydrocarbazoles incorporating 5-arylidene-4-thiazolinones as potential antileukemia and antilymphoma targeting tyrosine kinase and tubulin polymerase enzymes: Design, synthesis, structural, biological and molecular docking studies

Synthesis and Biological Activities of C1-Substituted Acylhydrazone β-Carboline Analogues as Antifungal Candidates

Contact Info

Product

Resources

About